Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT sub(2C) agonists

This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5- HT sub(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT sub(2A) and 5-HT sub(2B) receptors. Compound 11 was active in in...

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Published inBioorganic & medicinal chemistry letters Vol. 19; no. 18; pp. 5346 - 5350
Main Authors Andrews, Mark D, Green, Martin P, Allerton, Charlotte MN, Batchelor, David V, Blagg, Julian, Brown, Alan D, Gordon, David W, McMurray, Gordon, Millns, Daniel J, Nichols, Carly L, Watson, Lesa
Format Journal Article
LanguageEnglish
Published 15.09.2009
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Summary:This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5- HT sub(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT sub(2A) and 5-HT sub(2B) receptors. Compound 11 was active in in vivo models of stress urinary incontinence.
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2009.07.133